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Cat. No. Name Size Price Add Cart
KI1057E-3810QuoteQuote

Chemical Characteristic

Product NameE-3810
CAS No.117976-90-6
Molecular Weight 443.49
FormulaC26H25N3O4
Chemical Name6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide
Smiles[Na] C1(Nc2c(N1)cccc2)S(=O)Cc1c(c(ccn1)OCCCOC)C
Chemical Structure

Biological activities

E-3810 is a novel dual inhibitor of the VEGF and FGF receptors. E-3810 potently and selectively prevents the activities of VEGFR-1, VEGFR-2, and VEGFR-3 and FGFR-1 and FGFR -2 kinases in the nanomolar range. The IC50 of E-3810 is 7, 25, and 10 nM against VEGFR-1, VEGFR-2, and VEGFR-3, respectively. In addition, E-3810 inhibits FGFR-1 and FGFR-2 with IC50 of 17.5 and 82.5 nM, respectively. E-3810 also prevents c-Kit, PDGFR-α and PDGFR-β with IC50 of 0.5, 0.17 and 0.5 µM, respectively. E-3810 in the low nanomolar range inhibits the ligand-dependent phosphorylation of VEGFR-2 and FGFR-1 in HUVEC cells, in a dose-dependent fashion. In vitro, E-3810 potently suppresses the proliferation of VEGF and bFGF-stimulated HUVEC with IC50 of 40 and 50 nM, respectively.[1] Compared with the response in vehicle-treated mice, E-3810, at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits the bFGF induced angiogenic growth. E-3810 exhibits a broad spectrum of activity in the tested xenografts including HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas with dose-dependent inhibition of tumor growth. E-3810 induces vascular regression in human renal carcinoma xenografts.[1] The combination of E-3810 with paclitaxel reveals a striking activity with complete, lasting tumor regression in MDA-MB-231 triple-negative breast cancer xenograft model and MX-1 triple negative breast xenograft.[2]

Protocols

In vitro E-3810 is dissolved in 100% DMSO at a final concentration of 10 mM for in vitro treatment.[1]

References

[1] Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011, 71(4): 1396-1405.
[2] Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with paclitaxel inhibits the growth of advanced- stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2012.

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Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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